Sedatives/Hypnotics Flashcards
1
Q
Medications that cause insomnia
A
ETOH BB CCB Bronchodilators Caffeine Corticosteroids Decongestants Antidepressants Thyroids Anticonvulsants High BP Meds
2
Q
Treatment Duration of Insomnia
A
4-5 weeks per FDA lowest dose shortest duration DC gradually Rebound Effects Use Short Half-Life Drugs
3
Q
FDA Approved Drug Treatment for Insomnia
A
- Benzo’s
- Non Benzo’s (GABA drugs)
- Melatonin
- TCA/Histamine
- Dual Orexin Receptor Antagonist
4
Q
Off Label Drug Treatment for Insomnia
A
- Antidepressants
- Antipsychotics (with specific comorbids)
- Anticonvulsants (with specific comorbids)
- Antihistamines
5
Q
How Benzo’s and ZDrugs work
A
- Benzo’s working through GABA neurons resulting in HYPERpolarization of the cell
- GABA serves as an inhibitory inhibitor in the CNS, decreasing neuronal excitability
- Benzo’s cause sedation, decreased anxiety, muscle relaxant, retrograde amnesia
- ZDrugs (non benzo’s) are psychoactive drugs (benzo-like) and are very similar in side effects, risks, and benefits
- However, they have different chemical structure and differ on a molecular level
6
Q
Important Notes on Benzo’s
A
- Causes next day drowsiness
- Contraindication in pregnancy and breast feeding
- Should NOT BE USED with sleep apnea, pulmonary disease, or respiratory illness BECAUSE depresses respirations
- Schedule IV Drug
- Only use in healthy adults for short periods of time
7
Q
Ramelteon
A
- FDA approved
- Used: sleep onset (latency)
- Melatonin Receptor
- 8mg
- Effectiveness is modest
- Not habit forming
- Still has few side effects?
8
Q
Doxepin
A
- FDA approved
- Used: Sleep maintenance
- TCA/Histamine-1 Receptor Antagonist
- 3mg, 6mg
- VERY favorable for adults/elderly
- Other TCA’s like amitriptyline and nortriptyline should only be used for insomnia WITH comorbid of depression, fibromyalgia, neuropathic pain
9
Q
Side Effects of Benzo’s
A
- DAYTIME SEDATION
- Decreased reaction time
- Cognitive impairment and memory problems
- Unsteady gait leading to ataxia and falls
- Risk of tolerance
- Risk of withdrawal (+rebound insomnia)
- Risk of abuse (no sleep apnea, substance abuse)
10
Q
Non-Benzo’s (ZDrugs)
A
Zolpidem
- rebound not associated
- duration 8 hours
Zolpidem ER
- not limited to short term use
- duration 8 hours?
Zaleplon
- Not apparent withdrawal symptoms, daytime drowsiness/anxiety/psychomotor impairment
- Duration 4 hours
Eszopiclone
Ramelteon
11
Q
Non-Benzo’s (ZDrugs) *****
Eszopiclone
A
- Half life 6 hours
- Approved for insomnia, sleep onset (latency), maintenance
- Especially good for onset bc long half life
- Not limited to short term use
- Should not exceed 2mg in patients taking CYP3A4 drugs
- Delayed absorption/onset with meals
- CAN CAUSE METALLIC TASTE ESPECIALLY WITH HIGH DOSES
- Duration 8 hours
12
Q
Non-Benzo’s (ZDrugs) *****
Ramelteon
A
- Half life 2-5 hours
- Approved for insomnia, sleep onset
- Not limited to short term use
- melatonin receptor
- Not a controlled substance
- CYP1A2 AVOID use with fluvoxamine is contraindicated
- Food delays absorption/onset
- Duration 8 hours
- ONLY FDA DRUG THAT IS NOT A CONTROLLED SUBSTANCE BC NO POTENTIAL FOR ABUSE OR WITHDRAWAL
13
Q
Side Effects of ZDrugs
A
- Memory Loss
- Dizziness
- Disinhibition
- GI Upset
- Hallucinations
ALL ZDRUGS HAVE DELAYED ABSORPTION WITH FOOD
14
Q
Benefits of NON- Benzo’s
A
- Bind to subtypes of GABA receptors that specifically modulate sleep and there are though to have less unwanted side effects
- Tolerance and abuse have shown not to be major concern in general population
- Generally, shorter duration of action than most benzo’s and less like to cause sedation the next day
15
Q
Disadvantages of NON-Benzo’s
A
Complex Sleep Behaviors
- Sleep walking
- Sleep driving
- Engaging in activities before fully awake
( esp. with zolpidem sublingual and mist spray )
16
Q
Antidepressants for Insomnia
A
Commonly used by NOT FDA approved
- Trazodone: SSRI (can cause priapism which is persistent, painful erection)
- Amitriptyline: TCA
- Mirtazapine: Alpha 2 Antagonist
All usually given at much lower dosing than depression
FDA APPROVED
- Doxepin: TCA
17
Q
Key Clinicals for Benzo’s and Insomnia
A
- Benzo’s have greater improvement in 1st week then intermediate improvement in next 3-8 weeks (non pharm thought to be just as beneficial during this time)
- Drug therapy for insomnia should be limited to 4-5 weeks while learning CBTI treatment
18
Q
Key Clinicals for ZDrugs and Insomnia
A
- Caution in elderly, can cause falls
- Sedation increases if taken with other sedating drugs like etoh, antihistamines, benzos
- Avoid with respiratory depression or respiratory compromise
- CYP450 inhibitors (macrolides) increase ZDrug sedation
- CYP450 INDUCERS (phenytoin) diminish sedative effect
- Use short term: 4 weeks, longer can cause dependence
